期刊
CARBOHYDRATE POLYMERS
卷 212, 期 -, 页码 252-259出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2019.02.041
关键词
Hydroxypropyl-beta-cyclodextrin; Inclusion complex; Molecular modeling; Analytical method by LC-MS; Bioavailability
资金
- Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India
Niclosamide, previously used as an anthelmintic drug is currently being repurposed for its anticancer activity. Niclosamide is a brick like biopharmaceutical classification system (BCS) class II drug with poor aqueous solubility and dissolution consequently leading to low bioavailability. By considering the physicochemical properties and geometry of niclosamide, inclusion complex with cyclodextrin was prepared by freeze drying method and characterized using FT-IR, DSC, PXRD, and (HNMR)-H-1. In silico molecular modeling study was performed to study the possible interactions between niclosamide and cyclodextrin. The anticancer activity of niclosamide formulation was evaluated through in vitro cell cytotoxicity study using various cancer cell lines. The potential of niclosamide complex for improvement of the bioavailability was evaluated in male BALB/c mice. In vitro cytotoxicity studies indicated significantly higher cytotoxicity at lower concentrations and the pharmacokinetic studies showed significant improvement in C-max and T-max of niclosamide from cyclodextrin complex in comparison to pure niclosamide alone.
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